• Title/Summary/Keyword: synthetic activity

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The Effect of $17{\beta}-Estradiol$ on the Gene Expression of IGF-I and Bone Matrix Protein in the Osteoblast-Like Cell (골아세포의 IGF-I 유전자 발현 및 골기질 단백질에 대한 $17{\beta}-estradiol$의 영향)

  • Yang, Won-Suk;Lee, Jae-Mok;Suh, Jo-Young
    • Journal of Periodontal and Implant Science
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    • v.30 no.2
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    • pp.375-390
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    • 2000
  • The purpose of this study is to evaluate the expression ofIGF-I, considered as the mediator of action of estrogen, and IGF-IA and IGF-IB, alternative slicing form of IGF-I, using $17{\beta}-estradiol$ in MC3T3-E1 cells. We observed the effect on type I collagen and osteopontin gene expression and DNA synthetic activity of MC3T3-E1 cells, added by estrogen, IGF-I and combination and the interactionon proliferation and differentiation of MC3T3-E1 cells. The results were as follows :RT-PCR experiment for observing timedependantIGF-I gene expression patternshowed IGF-IA and IB gene expression in both of control and test group. In these IGF-IA gene expression was appeared predominantly. In control, IGF-I geneexpression level was maintained until 24hr and then decreased gradually. In testgroup, IGF-I gene expression level increased as time goes by. Experiment measuring DNA synthetic activity, as it is added by $17{\beta}-estradiol$, IGF-I and combination, showed that first day , there was the tendency of more increase of synthetic activity in all test group than control but no statical significance(P>0.05), and third day, there was more increase of DNA synthetic activity in $17{\beta}-estradiol$ group and combination group and it was statically significant. (P<0.005) Experiment for observing type I collagen gene expression pattern showed more increase of expression in $17{\beta}-estradiol$ group than control and no significant difference in IGF-I group and combination group. Experiment for observing osteopontin gene expression pattern showed no significant difference in control and test group. In conclusion, $17{\beta}-estradiol$ in MC3T3- E1 cells increased IGF-I gene and DNA synthetic activity simultaneously, therefore it appeared that IGF-I is related to the action of estrogen. Combination treatment of IGF-I and $17{\beta}-estradiol$ has effect on cell proliferation but this effect is lower than IGF-I or $17{\beta}-estradiol$ alone. However, combination treatment has not great effect on type I collagen or osteopontin gene expression thus little effect of cell differentiation.

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Study on Lifespan Extension Effect of Leonurine and its Synthetic Fragmental Analogs on Caenorhabditis elegans (예쁜꼬마선충을 이용한 레오누린과 그 합성 분절 유도체의 수명연장 효과 연구)

  • Cha, Dong Seok;Han, Young Taek
    • YAKHAK HOEJI
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    • v.60 no.3
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    • pp.141-145
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    • 2016
  • The current study was conducted to evaluate the lifespan extension effects of leonurine and its synthetic fragmental analogs using Caenohabditis elegans model system. Leonurine significantly prolonged the lifespan of C. elegans in a dose-dependent manner. To dissect the structure-activity relationship between leonurine and lifespan extension activity, seven novel fragmental analogs were synthesized and evaluated. Our study revealed that benzoate part of leonurine is responsible for its lifespan extension property rather than quanidine moiety.

Multicatalytic Alkaline Serine Pretense from the Psychrotrophic Bacillus amyloliquefaciens S94

  • Son, Eui-Sun;Kim, Jong-Il
    • Journal of Microbiology
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    • v.41 no.1
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    • pp.58-62
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    • 2003
  • An extracellular pretense of Bacillus amyloliquefaciens S94 was purified to apparent homogeneity. The enzyme activity was strongly inhibited by general inhibitor for serine protease, PMSF, suggesting that the enzyme is a serine pretense. The purified enzyme activity was inhibited by leucine peptidase inhibitor, bestatin, suggesting that the enzyme is a leucine endopeptidase. The maximum proteolytic activity against different protein substrates occurred at pH 10, 45$^{\circ}C$ (protein substrate) and pH 8, 45$^{\circ}C$ (synthetic substrate). The purified enzyme was specific in that it readily hydrolyBed substrates with Leu or Lys residues at P$_1$ site. The pretense had characteristics of a cold-adapted protein, which was more active for the hydrolysis of synthetic substrate in the range of 15$^{\circ}C$ to 45$^{\circ}C$, specially at low temperature.

Identification of Antimicrobial Peptide Hexamers against Oral Pathogens through Rapid Screening of a Synthetic Combinatorial Peptide Library

  • Song, Je-Seon;Cho, Kyung Joo;Kim, Joungmok;Kim, Jeong Hee
    • International Journal of Oral Biology
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    • v.39 no.4
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    • pp.169-176
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    • 2014
  • A positional scanning synthetic peptide combinatorial library (PS-SCL) was screened in order to identify antimicrobial peptides against the cariogenic oral bacteria, Streptococcus mutans. Activity against Streptococcus gordonii and Aggregatibacter actinomycetemcomitans was also examined. The library was comprised of six sub-libraries with the format $O_{(1-6)}XXXXX-NH_2$, where O represents one of 19 amino acids (excluding cysteine) and X represents equimolar mixture of these. Each sub-library was tested for antimicrobial activity against S. mutans and evaluated for antimicrobial activity against S. gordonii and A. actinomycetemcomitans. The effect of peptides was observed using transmission electron microscopy (TEM). Two semi-mixture peptides, RXXXXN-$NH_2$ (pep-1) and WXXXXN-$NH_2$ (pep-2), and one positioned peptide, RRRWRN-$NH_2$ (pep-3), were identified. Pep-1 and pep-2 showed significant antimicrobial activity against Gram positive bacteria (S. mutans and S. gordonii), but not against Gram negative bacteria (A. actinomycetemcomitans). However, pep-3 showed very low antimicrobial activity against all three bacteria. Pep-3 did not form an amphiphilic ${\alpha}$-helix, which is a required structure for most antimicrobial peptides. Pep-1 and pep-2 were able to disrupt the membrane of S. mutans. Small libraries of biochemically-constrained peptides can be used to generate antimicrobial peptides against S. mutans and other oral microbes. Peptides derived from such libraries may be candidate antimicrobial agents for the treatment of oral microorganisms.

Chemical Synthesis and Determination of Biological Activity of the Epidermal Growth Factor-Like Domain of Mouse Betacellulin

  • Shin, Song-Yub;Kang, Shin-Won;Ha, Jong-Myung
    • BMB Reports
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    • v.28 no.2
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    • pp.87-93
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    • 1995
  • To investigate the biological functions of the EGF-like domain of mouse betacellulin (BTC), mouse BTC(33-80), a 48-residue peptide corresponding to the EGF-like domain, was synthesized by stepwise solidphase methods using a 9-fluorenylmethoxycarbonyl (Fmoc) strategy. The homogeneity of synthetic mouse BTC(33-80) was confirmed by analytical reversed phase (RP)-HPLC, amimo acid analysis, and fast atom bombardment mass spectrometer (FAB-MS). Three disulfide bond pairings of synthetic mouse BTC(33-80) were established by amino acid analysis of cysteine-containing fragments derived from thermolytic digestion. These were consistent with the pairings of EGF and transforming growth factor ($TGF-{\alpha}$). The EGF-Iike domain of mouse BTC showed equipotent activity in both EGF-receptor binding on A-431 epidermoid carcinoma cells, and mitogenesis on NIH-3T3 fibroblast cells, as compared with authentic h-EGF. Results suggest that the EGF-Iike domain of BTC plays a significant role in mitogenic activity with an EGF-receptor mediated system.

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Antioxidant Activity of γ-Oryzanol and Synthetic Phenolic Compounds in an Oil/Water (O/W) Emulsion System

  • Kim, Joo-Shin
    • Preventive Nutrition and Food Science
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    • v.12 no.3
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    • pp.173-176
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    • 2007
  • ${\gamma}-Oryzanol$ is one of the chain breaking antioxidants. Both sterol (triterpene) and phenolic hydroxyl groups in the structure of ${\gamma}-oryzanol$ may be responsible for its antioxidative function. We hypothesize that ${\gamma}-oryzanol$ is more effective in preventing the autoxidation of polyunsaturated fatty acid (PUFA) than the synthetic phenolic compounds in an oil/water (O/W) emulsion system. The antioxidative effectiveness of different concentrations of ${\gamma}-oryzanol$ and synthetic antioxidants was evaluated at different incubation times (0, 4, 8, 16, and 32 h) by measuring both the formation of hydroperoxides and the decomposition product of hydroperoxides (hexanal) in each emulsion system. Overall, the order of effectiveness of various antioxidants for inhibiting the formation of hydroperoxide in the O/W emulsion was: ${\gamma}-oryzanol$> tert-butylhydroquinone (TBHQ)> butylated hydroxytoluene (BHT)> butylated hydroxyanisole (BHA). O/W emulsion with selective lower concentrations of ${\gamma}-oryzanol$ showed better effectiveness than that with higher concentration of synthetic antioxidants. However, the ability of both ${\gamma}-oryzanol$ and synthetic antioxidants to decompose hydroperoxide was similar. ${\gamma}-Oryzanol$ was more effective antioxidant than the synthetic phenolic compounds in preventing the formation of hydroperoxide in the O/W emulsion system.

Synthesis and Biological Activity of Fungal Metabolite, 4-Hydroxy-3-(3'-Methyl-2'-Butenyl)-Benzoic Acid

  • Kim, Hye-Jin;Kwon, Ho-Jeong
    • Journal of Microbiology and Biotechnology
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    • v.17 no.3
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    • pp.543-545
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    • 2007
  • 4-Hydroxy-3-(3'-methyl-2'-butenyl)-benzoic acid (HMBA) was previously isolated from Curvularia sp. KF119 as a cell-cycle inhibitor. However, the present study used a novel and practical synthetic method to prepare a large quantity of HMBA. The synthetic HMBA was found to inhibit the cell-cycle progression of HeLa cells with a comparable potency to the natural fungal metabolite. The inhibition of the cell-cycle progression by the synthetic HMBA involved both the activation of $p21^{WAF1}$ and the inhibition of cyclin D1 expression in the cells. Consequently, this new synthetic procedure provides an easy and convenient way to produce or manipulate the original fungal metabolite.

Antibacterial, antioxidant and antitumor activities of mushroom mycelium mixed culture extracts (버섯 균사체 혼합 배양 추출물의 항균, 항산화 및 항암 활성)

  • Kim, Man-Cheol;Kim, Ju-Sang;Heo, Moon-Soo
    • KSBB Journal
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    • v.23 no.2
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    • pp.158-163
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    • 2008
  • In this study, we have investigated the antibacterial, antioxidant, and antitumor activities of mycelium cultural extract from mushroom. Mushroom mycelium was grown in a synthetic liquid media such as PD broth, YM broth or citrus extracts. In antibacterial activity test, the best result was achieved when mycelium cultural extracts from Phellinus linteus and Coriolus versicolor were incubated together on YM broth. On the other hand, mushroom mycelium cultured on citrus extracts showed better activity than that on PD broth. We have also tested the antioxidant activity at concentration up to 10 mg of mycelium cultural extract/mL. The more it is in higher concentration, the more the activity increases. The higher antioxidant activity was observed both on PD broth containing the Phellinus linteus and Coriolus versicolor mycelium and citrus extract containing the same. The complex culture extracts obtained from the synthetic medium and citrus extract medium showed 10-89% of the 1,1-diphenyl-2-picrylhydrazyl radical scavenger activity. The antitumor activity of mycelium cultural extract was examined by using MTT assay on A549 cells. Mushroom mycelium cultured on citrus extracts showed interestingly higher antitumor activity than that on synthetic liquid media.

Synthesis and Anti-inflammatory Activity of Fenbufen-Acetaminophen Ester (Fenbufen-Acetaminophen Ester의 합성 및 항염 작용)

  • 서정진;이종욱
    • YAKHAK HOEJI
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    • v.28 no.1
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    • pp.17-20
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    • 1984
  • Synthetic procedures to synthesize fenbufen-acetaminophen ester were searched by acid chloride method, DCC method and mixed acid anhydride method. The compound was synthesized by DCC method and mixed acid anhydride method but could not be synthesized by acid chloride method. Its anti-inflammatory activity was superior to acetaminophen and similar to fenbufen.

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Structure-Activity Relationship Study of Asiatic Acid Derivatives for New Wound Healing Agent

  • Jeong, Byeong-Seon
    • Archives of Pharmacal Research
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    • v.29 no.7
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    • pp.556-562
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    • 2006
  • Ten semi-synthetic derivatives of asiatic acid were prepared and their wound healing effects were evaluated by employing a tensile strength assay and a wound area assay. Among them, ethoxymethyl 2-oxo-3,23-isopropylidene-asiatate (12) showed the strongest and the fastest wound healing activity. Furthermore, it left the smallest scar after healing.